Peng Xiaoyan, Dai Yuxing, Chen Jianwen, Lu Jing, Zhou Dan, Ge Fahuan, Liu Peiqing, Zhou Xue
Department of Pharmacognosy and Natural Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.
Guangdong Research Center for Supercritical Fluid Extraction of Chinese Medicine, Guangzhou 511458, China.
Pharmaceuticals (Basel). 2025 May 15;18(5):728. doi: 10.3390/ph18050728.
: Early studies indicated that the high content of tanshinone IIA (T-IIA) and rosmarinic acid (RA) in Diels f. Stib (SCT) gives them significant potential for development as therapeutic agents for ischemic stroke (IS). However, the extraction process and quality of the active ingredients from SCT are still big challenges, with present processes providing insufficient pharmacological effects. This study aims to identify the optimal extraction process and perform a quality characterization of the total tanshinones and phenolic acids extracted from SCT, as well as to elucidate the neuroprotective effect of these extracts. : The extraction process was optimized using an orthogonal experimental design (OED), and quality characterization was performed using HPLC, UV, and LC-MS. The neuroprotective effect of the extracted tanshinones and phenolic acids was studied using the middle cerebral artery occlusion (MCAO) paradigm, and its underlying mechanism was revealed through RNA-seq analysis combined with network pharmacology. : The optimal extraction pressure of total tanshinones was 60 MPa, while the extraction temperature and time for total phenolic acids were 4 °C and 25 min, respectively. In these extracts, the total tanshinone and phenolic acid contents increased to 369.43 and 189.10 mg/g, respectively; 23 of the 19 tanshinones and 23 phenolic acids identified in this study have not been observed in previous studies. It was demonstrated that the combined extract had a promising neuroprotective effect against IS; RNA-seq combined with network pharmacology analysis indicated that the active compounds may regulate a series of core genes associated with signaling pathways to protect against IS. : The combined SCT extract studied in this research exerted neuroprotective effects on IS. In general, these findings improve our preliminary understanding of the chemical composition and bioactivity of SCT.
早期研究表明，甘肃丹参（SCT）中丹参酮IIA（T-IIA）和迷迭香酸（RA）含量较高，使其具有作为缺血性中风（IS）治疗药物开发的巨大潜力。然而，SCT活性成分的提取工艺和质量仍是巨大挑战，现有工艺的药理作用不足。本研究旨在确定最佳提取工艺，对从SCT中提取的总丹参酮和酚酸进行质量表征，并阐明这些提取物的神经保护作用。
采用正交试验设计（OED）优化提取工艺，并用高效液相色谱（HPLC）、紫外可见分光光度法（UV）和液相色谱-质谱联用（LC-MS）进行质量表征。采用大脑中动脉闭塞（MCAO）模型研究提取的丹参酮和酚酸的神经保护作用，并通过RNA测序（RNA-seq）分析结合网络药理学揭示其潜在机制。
总丹参酮的最佳提取压力为60MPa，而总酚酸的提取温度和时间分别为4℃和25分钟。在这些提取物中，总丹参酮和酚酸含量分别增至369.43和189.10mg/g；本研究鉴定出的19种丹参酮和23种酚酸中有23种在以往研究中未被观察到。结果表明，该联合提取物对IS具有良好的神经保护作用；RNA-seq结合网络药理学分析表明，活性化合物可能调节一系列与信号通路相关的核心基因以预防IS。
本研究中所研究的SCT联合提取物对IS具有神经保护作用。总体而言，这些发现增进了我们对SCT化学成分和生物活性的初步了解。
